Target
High affinity nerve growth factor receptor
Ligand
BDBM406184
Substrate
n/a
Meas. Tech.
Kinase Binding Assay
IC50
<100±n/a nM
Citation
 Allen, SAndrews, SWBlake, JFBrandhuber, BJHaas, JJiang, YKercher, TKolakowski, GRThomas, AAWinski, SL Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain US Patent  US10351575 Publication Date 7/16/2019 
Target
Name:
High affinity nerve growth factor receptor
Synonyms:
2.7.10.1 | MTC | NTRK1 | NTRK1/NTRK2 | NTRK1_HUMAN | Nerve growth factor receptor Trk-A | Neurotrophic tyrosine kinase receptor type 1 | Neurotrophic tyrosine kinase receptor type 1 (TrkA) | Synonyms=MTC | TRK | TRK1-transforming tyrosine kinase protein | TRKA | TRKA GN | Trk-A | Tropomyosin alpha-3 chain/High affinity nerve growth factor receptor | Tropomyosin-related kinase A | Tropomyosin-related kinase A (TrkA) | Tyrosine kinase receptor | Tyrosine kinase receptor (Trk) | Tyrosine kinase receptor A | Tyrosine kinase receptor A (Trk A) | Tyrosine kinase receptor A (Trk-A) | Tyrosine kinase receptor A (TrkA) | gp140trk | p140-TrkA
Type:
n/a
Mol. Mass.:
87498.18
Organism:
Homo sapiens (Human)
Description:
P04629
Residue:
796
Sequence:
MLRGGRRGQLGWHSWAAGPGSLLAWLILASAGAAPCPDACCPHGSSGLRCTRDGALDSLHHLPGAENLTELYIENQQHLQHLELRDLRGLGELRNLTIVKSGLRFVAPDAFHFTPRLSRLNLSFNALESLSWKTVQGLSLQELVLSGNPLHCSCALRWLQRWEEEGLGGVPEQKLQCHGQGPLAHMPNASCGVPTLKVQVPNASVDVGDDVLLRCQVEGRGLEQAGWILTELEQSATVMKSGGLPSLGLTLANVTSDLNRKNVTCWAENDVGRAEVSVQVNVSFPASVQLHTAVEMHHWCIPFSVDGQPAPSLRWLFNGSVLNETSFIFTEFLEPAANETVRHGCLRLNQPTHVNNGNYTLLAANPFGQASASIMAAFMDNPFEFNPEDPIPVSFSPVDTNSTSGDPVEKKDETPFGVSVAVGLAVFACLFLSTLLLVLNKCGRRNKFGINRPAVLAPEDGLAMSLHFMTLGGSSLSPTEGKGSGLQGHIIENPQYFSDACVHHIKRRDIVLKWELGEGAFGKVFLAECHNLLPEQDKMLVAVKALKEASESARQDFQREAELLTMLQHQHIVRFFGVCTEGRPLLMVFEYMRHGDLNRFLRSHGPDAKLLAGGEDVAPGPLGLGQLLAVASQVAAGMVYLAGLHFVHRDLATRNCLVGQGLVVKIGDFGMSRDIYSTDYYRVGGRTMLPIRWMPPESILYRKFTTESDVWSFGVVLWEIFTYGKQPWYQLSNTEAIDCITQGRELERPRACPPEVYAIMRGCWQREPQQRHSIKDVHARLQALAQAPPVYLDVLG
  
Inhibitor
Name:
BDBM406184
Synonyms:
1-(4-methyl-3-(2- methylpyrimidin-5-yl)-1- phenyl-1H-pyrazol-5-yl)- 3-(1-oxo-2-(2,2,2- trifluoroethyl)-1,2,3,4- tetrahydroisoquinolin-4- yl)urea | US10351575, Example 130 | US10889589, EX. # 130
Type:
Small organic molecule
Emp. Form.:
C27H24F3N7O2
Mol. Mass.:
535.5204
SMILES:
Cc1c(NC(=O)NC2CN(CC(F)(F)F)C(=O)c3ccccc23)n(nc1-c1cnc(C)nc1)-c1ccccc1
Structure:
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